Acetylcholinesterase Inhibitory Activity of Uleine from Himatanthus lancifolius

2010 ◽  
Vol 65 (7-8) ◽  
pp. 440-444 ◽  
Author(s):  
Cláudia Seidl ◽  
Beatriz L. Correia ◽  
Andréa E. M. Stinghen ◽  
Cid A. M. Santos
Keyword(s):  
Inhibitory Activity ◽  
Colorimetric Method ◽  
Indole Alkaloid ◽  
Ethyl Acetate Fraction ◽  
Primary Treatment ◽  
Huperzine A ◽  
Ache Inhibition ◽  
Ache Inhibitors ◽  
Ache Inhibitory Activity ◽  
Layer Chromatography

Application of acetylcholinesterase (AChE) inhibitors is the primary treatment for Alzheimer’s disease. Alkaloids, such as physostigmine, galanthamine, and huperzine A, play an important role as AChE inhibitors. The aim of this work was to evaluate Himatanthus lancifolius (Muell. Arg.) Woodson, a Brazilian species of Apocynaceae, and its main indole alkaloid uleine, in order to identify new AChE inhibitors. The plant fluid extract, fractions, and uleine were tested for AChE inhibitory activity using Ellman’s colorimetric method for thin-layer chromatography (TLC), 96-well microplates, and also Marston’s TLC colorimetric method. Both TLC assays showed similar results. At 5 mg/mL, the fluid extract inhibited the AChE enzyme by (50.71 ± 8.2)%. The ethyl acetate fraction exhibited the highest level of AChE inhibition, followed by the dichloromethane fraction. The isolated alkaloid uleine displayed an IC50 value of 0.45 μM.

scholarly journals Evaluation of Acetylcholinesterase Inhibitory Activity of Fractions from Mahonia nepalensis (Berberidaceae) Extract

2017 ◽  
Vol 33 (2) ◽  
Author(s):  
Bui Thanh Tung ◽  
Phan Ke Son ◽  
Dang Kim Thu ◽  
Nguyen Thanh Hai ◽  
Nguyen Xuan Bach ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inhibitory Activity ◽  
Colorimetric Method ◽  
Dependent Manner ◽  
Etoh Extract ◽  
Ache Inhibitors ◽  
Ache Inhibitory Activity ◽  
Etoac Fraction ◽  
Promising Source

Acetylcholinesterase (AChE) is a key target in the treatment of Alzheimer’s disease. Principal role of AChE hydrolyzes the neurotransmiter acetylcholine. Medicinal plants are the potential source of AChE inhibitors. In this study, we studied the AChE inhibitory activities of extraction  Mahonia nepalensis. This medicianl plant was extracted with ethanol 96% and subsequently fractionated with n-hexane, ethyl acetate (EtOA) and n-butanol (n-BuOH) solvents. These fractions were evaluated the AChE inhibitory activity by Ellman’s colorimetric method.  Results showed that n-BuOH fraction had the strongest AChE inhibitory activity, followed by EtOH extract and the EtOAc fraction was the weakest. The n-BuOH fraction inhibited AChE activity in a dose-dependent manner with an IC50 value of 3.38 ± 0.07 μg/mL. Detailed kinetic analysis indicated that n-BuOH fraction was mixed inhibiton type with Ki value of 3.416 ± 0.05 µg/mL. Our  data suggests that  the  Mahonia nepalensis may be  a  promising  source  of  AChE  inhibitors  for Alzheimer’s disease.

scholarly journals SYZYGIUM CUMINI (L.) SKEELS LEAF EXTRACT FRACTIONS AS ARGINASE INHIBITORS AND THE EFFECTS OF TANNINS ON THEIR ACTIVITY

2020 ◽  
pp. 268-270
Author(s):  
ARI ARIEFAH HIDAYATI ◽  
BERNA ELYA ◽  
RANI SAURIASARI
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Colorimetric Method ◽  
Ethyl Acetate Fraction ◽  
Precipitation Method ◽  
Total Phenolic ◽  
Syzygium Cumini ◽  
Methanol Fraction ◽  
Phenolic And Flavonoid

Objective: Arginase inhibition could be a potential therapeutic approach for endothelial dysfunction. Syzygium cumini (L.) Skeels leaves containphenolic acids and flavonoids, which have been predicted to exhibit arginase inhibitory activity. Moreover, these leaves contain tannins, which canform complexes with enzymes and lead to false-positive results during biological testing. Therefore, this study was conducted to evaluate the arginaseinhibitory activity of S. cumini leaf extract and fractions as well as to elucidate the effects of tannins on this activity.Methods: S. cumini leaves were fractionated using n-hexane, ethyl acetate, and methanol. A colorimetric method was employed to evaluate arginaseinhibitory activity. Tannin elimination was performed through the gelatin precipitation method. Total phenolic and flavonoid contents of the fractionswere calculated using the Folin–Ciocalteu and aluminum chloride methods, respectively.Results: Ethyl acetate and methanol fractions showed arginase inhibitory activity with half-maximal inhibitory concentrations (IC50) of 46.96 and15.35 μg/mL, respectively. The methanol fraction was positive for tannins. After tannin elimination, this fraction exhibited less potent arginaseinhibitory activity, with an IC50 value of 53.03 μg/mL. The ethyl acetate fraction showed higher total phenolic and flavonoid contents than the methanolfraction.Conclusion: Tannins affected the arginase inhibitory activity of the methanol fraction of S. cumini leaves; however, the ethyl acetate fraction did notcontain tannins and could inhibit arginase activity.

scholarly journals Triterpenes from Warszewiczia coccinea (Rubiaceae) as Inhibitors of Acetylcholinesterase

2009 ◽  
Vol 4 (10) ◽  
pp. 1934578X0900401
Author(s):  
Angela I. Calderón ◽  
Johayra Simithy ◽  
Giuliana Quaggio ◽  
Alex Espinosa ◽  
Jose Luis López-Pérez ◽  
...  
Keyword(s):  
Free Radical ◽  
Thin Layer ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Spectroscopic Methods ◽  
Ache Inhibitors ◽  
Ache Inhibitory Activity ◽  
Stem Extract ◽  
Layer Chromatography ◽  
Free Radical Scavenging Activities

Seventy-six plant extracts from the Panamanian flora have been screened for acetylcholinesterase (AChE) inhibitors by thin-layer chromatography (TLC) bioautography. The most promising extracts with AChE inhibitory and free radical scavenging activities at 100 μg were those of Tabernaemontana panamensis (Markgr., Boiteau & L. Allorge) Leeuwenb., Pentagonia macrophylla Benth., and Warszewiczia coccinea (Vahl) Klotzsch. Bioguided fractionation of W. coccinea stem extract afforded two triterpenes, 3β,6β,19α-trihydroxy-urs-12-en-28-oic acid (1) and 3β,6β-dihydroxy-olean-12-en-28-oic acid (sumaresinolic acid) (2), with AChE inhibitory activity. Their structures were determined by spectroscopic methods. This is the first report of these bioactive triterpenes in W. coccinea.

Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity

1991 ◽  
Vol 34 (12) ◽  
pp. 3399-3402 ◽  
Author(s):  
Alan P. Kozikowski ◽  
Chris P. Miller ◽  
Fumio Yamada ◽  
Yuan Ping Pang ◽  
Jacqueline H. Miller ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Huperzine A ◽  
Ache Inhibitory Activity

Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

2014 ◽  
Vol 69 (1) ◽  
Author(s):  
Saleh Nazifi Ibrahim ◽  
Farediah Ahmad
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Microplate Assay ◽  
Synthetic Compounds ◽  
Ache Inhibitory Activity ◽  
Weak Activity ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation

A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration compared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay.

scholarly journals Protective Evaluation of Compounds Extracted from Root of Rhodiola rosea L. against Methylglyoxal-Induced Toxicity in a Neuronal Cell Line

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2801
Author(s):  
Cheng-Hao Wang ◽  
Safwan Safwan ◽  
Min-Chi Cheng ◽  
Te-Yu Liao ◽  
Lin-Chen Cheng ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Neuronal Cell ◽  
Ethyl Acetate Fraction ◽  
Rhodiola Rosea ◽  
Neuroprotective Activity ◽  
Structure Identification ◽  
N2a Cells ◽  
Ache Inhibitory Activity ◽  
Induced Apoptosis

Rhodiola rosea L. (R. rosea) is one of the most beneficial medicinal plants and it is studied as an adaptogen. This study aims to evaluate the neuroprotective activity of compounds extracted from the root of R. rosea against methylglyoxal (MG)-induced apoptosis in neuro-2A (N2A) cells. The root of R. rosea was extracted with ethanol and partitioned with water, ethyl acetate, and n-butanol fractions to evaluate acetylcholinesterase (AChE) inhibitory activity and neuroprotective activity. The ethyl acetate fraction exhibited the highest values of AChE inhibitory activity (49.2% ± 3%) and cell viability (50.7% ± 4.8%) for neuroprotection. The structure identification of the most potential fraction (ethyl acetate fraction) revealed 15 compounds, consisting of three tannins, five flavonoids, and seven phenolics by infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. All compounds were evaluated for their neuroprotective activity. Salidroside had the most potential neuroprotective activity. Gallic acid and methyl gallate had potential cytotoxicity in N2A cells. This study showed that R. rosea might have potential neuroprotective activities.

scholarly journals Antioxidant and Anticholinesterase Potential of SixThymusSpecies

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Marija Kindl ◽  
Biljana Blažeković ◽  
Franz Bucar ◽  
Sanda Vladimir-Knežević
Keyword(s):  
Colorimetric Method ◽  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Dependent Manner ◽  
Ache Inhibitors ◽  
Antioxidant Effectiveness ◽  
Total Antioxidant ◽  
Ache Inhibitory Activity ◽  
Inhibit Lipid Peroxidation ◽  
Dose Dependent

The present study aimed to evaluate antioxidant and acetylcholinesterase (AChE) inhibitory activities of the ethanolic extracts of six selectedThymusspecies growing in Croatia (T. longicaulis,T. praecoxsubsp.polytrichus,T. pulegioides,T. serpyllumsubsp.serpyllum,T. striatus, andT. vulgaris). Antioxidant effectiveness was assessed using six different assays, in comparison with rosmarinic acid, luteolin, and reference antioxidants. All testedThymusextracts possessed DPPH (IC50= 3–6 μg/mL) and nitric oxide (IC50= 70–177 μg/mL) free radical scavenging activities, strong reducing properties (IC50= 11–15 μg/mL), ferrous ion chelating activity (IC50= 126–389 μg/mL), ability to inhibit lipid peroxidation (IC50= 34–80 μg/mL), and high total antioxidant capacities (238–294 mg AAE/g). AChE inhibitory activity was examined using Ellman's colorimetric method and all tested extracts showed anti-AChE activity in a dose dependent manner. The values of 10–28%, 23–39%, and 64–86% were obtained for tested concentrations of 0.25, 0.5, and 1 mg/mL, respectively. Additionally, the contents of total hydroxycinnamic derivatives, flavonoids, and tannins in dried plant samples were determined spectrophotometrically. Our results highlightedThymusspecies as a rich source of natural antioxidants and AChE inhibitors that could be useful in preventing and treating Alzheimer’s disease and other neurodegenerative disorders.

Design, One-Pot Synthesis, and Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-Triazin-7-One Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

2014 ◽  
Vol 884-885 ◽  
pp. 607-610
Author(s):  
Si Jie Liu ◽  
Lan Xiang Shi ◽  
Jing Yu He ◽  
Li Bo Cui
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Colorimetric Assay ◽  
Acetylcholinesterase Inhibitors ◽  
Positive Control ◽  
Huperzine A ◽  
One Pot ◽  
Control Drug ◽  
Ache Inhibitory Activity ◽  
Methyl Pyrrolidone

In order to study the the structure-AChE inhibitory activity relationships of 7H-thiazolo [3,2-b]-1,2,4-triazin-7-one derivatives, the 7H-thiazolo[3,2-b]-1,2,4-triazin-7-ones were designed by molecular docking, and readily prepared via a one-pot reaction in N-methyl pyrrolidone hydrosulfate ([Hnmp]HSO4) lonic liquid. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10μM.

scholarly journals 1,3,5-Triazine Nitrogen Mustards with Different Peptide Group as Innovative Candidates for AChE and BACE1 Inhibitors

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3942
Author(s):  
Dawid Maliszewski ◽  
Agnieszka Wróbel ◽  
Beata Kolesińska ◽  
Justyna Frączyk ◽  
Danuta Drozdowska
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Colorimetric Method ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Triazine Ring ◽  
Peptide Group ◽  
Nitrogen Mustards ◽  
Ache Inhibitory Activity ◽  
Bace1 Inhibition

A series of new analogs of nitrogen mustards (4a–4h) containing the 1,3,5-triazine ring substituted with dipeptide residue were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and β-secretase (BACE1) enzymes. The AChE inhibitory activity studies were carried out using Ellman’s colorimetric method, and the BACE1 inhibitory activity studies were carried out using fluorescence resonance energy transfer (FRET). All compounds displayed considerable AChE and BACE1 inhibition. The most active against both AChE and BACE1 enzymes were compounds A and 4a, with an inhibitory concentration of AChE IC50 = 0.051 µM; 0.055 µM and BACE1 IC50 = 9.00 µM; 11.09 µM, respectively.

scholarly journals Synergistic Inhibition of Acetylcholinesterase by Alkaloids Derived from Stephaniae Tetrandrae Radix, Coptidis Rhizoma and Phellodendri Chinensis Cortex

Molecules ◽  
2019 ◽  
Vol 24 (24) ◽  
pp. 4567 ◽  
Author(s):  
Xiang-Peng Kong ◽  
Etta Y.L. Liu ◽  
Zhi-Cong Chen ◽  
Miranda Li Xu ◽  
Anna X.D. Yu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Simulation ◽  
Huperzine A ◽  
Ache Inhibition ◽  
Active Components ◽  
Molecular Docking Simulation ◽  
Synergistic Inhibition ◽  
Ache Inhibitory Activity ◽  
Coptidis Rhizoma ◽  
Main Components

Alkaloids having acetylcholinesterase (AChE) inhibitory activity are commonly found in traditional Chinese medicine (TCM); for example, berberine from Coptis chinensis, galantamine from Lycoris radiata, and huperzine A from Huperzia serrata. In practice of TCM, Stephaniae Tetrandrae Radix (STR) is often combined with Coptidis Rhizoma (CR) or Phellodendri Chinensis Cortex (PCC) as paired herbs during clinical application. Fangchinoline from STR and coptisine and/or berberine from CR and/or PCC are active alkaloids in inhibiting AChE. The traditional usage of paired herbs suggests the synergistic effect of fangchinoline–coptisine or fangchinoline–berberine pairing in AChE inhibition. HPLC was applied to identify the main components in herbal extracts of STR, CR, and PCC, and the AChE inhibition of their main components was determined by Ellman assay. The synergism of herb combination and active component combination was calculated by median-effect principle. Molecular docking was applied to investigate the underlying binding mechanisms of the active components with the AChE protein. It was found that fangchinoline showed AChE inhibitory potency; furthermore, fangchinoline–coptisine/berberine pairs (at ratios of 1:5, 1:2, 1:1, and 2:1) synergistically inhibited AChE; the combination index (CI) at different ratios was less than one when Fa = 0.5, suggesting synergistic inhibition of AChE. Furthermore, the molecular docking simulation supported this enzymatic inhibition. Therefore, fangchinoline–coptisine/berberine pairs, or their parental herbal mixtures, may potentially be developed as a possible therapeutic strategy for Alzheimer’s patients.

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